Source:http://linkedlifedata.com/resource/pubmed/id/19822427
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
22
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pubmed:dateCreated |
2009-10-26
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pubmed:abstractText |
The dapE-encoded N-succinyl-L,L-diaminopimelic acid desuccinylase (DapE) is a critical bacterial enzyme for the construction of the bacterial cell wall. A screen biased toward compounds containing zinc-binding groups (ZBG's) including thiols, carboxylic acids, boronic acids, phosphonates and hydroxamates has delivered a number of micromolar inhibitors of DapE from Haemophilus influenzae, including the low micromolar inhibitor L-captopril (IC(50)=3.3 microM, K(i)=1.8 microM). In vitro antimicrobial activity was demonstrated for L-captopril against Escherichia coli.
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pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical | |
pubmed:status |
MEDLINE
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pubmed:month |
Nov
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pubmed:issn |
1464-3405
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pubmed:author | |
pubmed:issnType |
Electronic
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pubmed:day |
15
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pubmed:volume |
19
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
6350-2
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pubmed:meshHeading |
pubmed-meshheading:19822427-Amidohydrolases,
pubmed-meshheading:19822427-Amino Acid Sequence,
pubmed-meshheading:19822427-Anti-Bacterial Agents,
pubmed-meshheading:19822427-Binding Sites,
pubmed-meshheading:19822427-Diaminopimelic Acid,
pubmed-meshheading:19822427-Enzyme Inhibitors,
pubmed-meshheading:19822427-Escherichia coli,
pubmed-meshheading:19822427-Haemophilus influenzae,
pubmed-meshheading:19822427-Microbial Sensitivity Tests,
pubmed-meshheading:19822427-Mutagenesis, Site-Directed,
pubmed-meshheading:19822427-Substrate Specificity
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pubmed:year |
2009
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pubmed:articleTitle |
Inhibitors of bacterial N-succinyl-L,L-diaminopimelic acid desuccinylase (DapE) and demonstration of in vitro antimicrobial activity.
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pubmed:affiliation |
Department of Chemistry, Loyola University, 6525 North Sheridan Road, Chicago, IL 60626, USA.
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pubmed:publicationType |
Journal Article,
Research Support, U.S. Gov't, Non-P.H.S.
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